Pirenzepine ophthalmic gel

a technology of pirenzepine and gel, which is applied in the field of aqueous ophthalmic pharmaceutical formulations, can solve the problems of limited clinical use of atropine as a therapy, inacceptable products, physical appearance problems,

Inactive Publication Date: 2006-08-24
VF PHARMA
View PDF14 Cites 22 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The clinical use of atropine as a therapy has been limited due to its ocular side effects including glare from pupillary dilation and blurred vision due to loss of accommodation.
However, work on a solution dosage form of pirenzepine indicated a physical appearance problem.
Thus, the accumulation of even a small amount of degradation product over the shelf-life of the sol

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pirenzepine ophthalmic gel

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0025] An aqueous ophthalmic gel of 2.0% pirenzepine for the treatment of myopia according to the present invention was prepared as follows:

TABLE 1Pirenzepine ophthalmic gel formulations.0.5%1.0%2.0%Ingredient(in mg / g)(in mg / g)(in mg / g)Pirenzepine dihydrochloride6.312.625.2(base equivalent)(5.0)(10.0)(20.0)Hydroxypropyl Methyl-Cellulose202020(K100M, Dow Chemical Co.)Sodium acetate0.400.400.40Benzalkonium chloride0.050.050.05Edetate disodium0.150.150.15Sodium chloride5.03.50.0Sodium Hydroxide (q.s. to pH)5.05.05.0Purified Water, q.s. to1.00 g1.00 g1.00 g

[0026] Part 1: Purified water was heated to 80-90° C. Hydroxypropyl methylcellulose (HPMC) was added and mixed until it was uniformly dispersed. The pH was adjusted to 5.0±1.0 with sodium hydroxide, but this was not a critical step and can be eliminated. After being placed in a pressure vessel, the mixture was sterilized at 121° C. for 30-45 minutes. In another embodiment, autoclaving is conducted under nitrogen when oxygen plays a ...

example 2

[0030] The ophthalmic pirenzepine gel preparation made in Example 1 was administered as follows (the ophthalmic tip of the dispensing mechanism did not touch any surface to avoid contamination). The lower lid of the eye to be administered was pulled down and a small amount of gel (approximately 0.25 inches) was applied to the inside of the eyelid. The gel was applied to the afflicted eye twice per day. A gel formulation in a target population of pediatric subjects was well tolerated.

example 3

[0031] Procedure for Viscosity Measurement: A Brookfield Cone and Plate Viscometer (Model RVDV-III+) was used to measure viscosity at about 20° C. and shear rate of 1 s−1. The viscosities of 0.5-2 g samples of various gels were measured. Gels with viscosities of 5,000 to less than 600,000 cps were tested with a CP52 spindle, and other spindles are used depending on the viscosities of the gels.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Temperatureaaaaaaaaaa
Frequencyaaaaaaaaaa
Concentrationaaaaaaaaaa
Login to view more

Abstract

It is a primary object of the present invention to provide an aqueous ophthalmic formulation, for treating myopia, comprising pirenzepine in combination with a pharmaceutically acceptable gel carrier.

Description

RELATED APPLICATIONS [0001] This application is a continuation of application Ser. No. 10 / 698,320, filed Oct. 31, 2003, which is a continuation of International Application No. PCT / US02 / 13823 filed May 1, 2002, designating the United States of America and published in English as WO 02 / 096418 on Dec. 5, 2002, which claims the benefit of U.S. Provisional Application No. 60 / 293,731 filed May 25, 2001, all of which are hereby expressly incorporated by reference in their entireties.FIELD OF THE INVENTION [0002] The present invention is in the field of aqueous ophthalmic pharmaceutical formulations. BACKGROUND OF THE INVENTION [0003] Myopia, axial elongation of the eye, affects a large proportion of the population. Commonly, the onset of myopia is during the grade school years and progresses until growth of the eye is completed. A pharmacologic therapy which prevents or retards the developmental abnormality of myopia would represent a major advance in the treatment of myopia. [0004] The p...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K31/551A61K9/14A61K9/00C07D471/04A61K31/205A61K31/42A61K31/5513A61K31/5517A61K47/02A61K47/18A61K47/38A61P27/02A61P43/00
CPCA61K9/0048A61K31/5513A61K31/5517A61K47/38A61P27/02A61P27/10A61P43/00A61K9/00
Inventor TAKRURI, HARUN
Owner VF PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap